The Current Opinion journals were developed out of the recognition that it is increasingly difficult for specialists to keep up to date with the expanding volume of information published in their subject. Elsevier’s Current Opinion journals comprise of 17 leading titles in life sciences and adjacent fields.

Current Opinion in Pharmacology

5-Year Impact Factor: 5.203
Issues per year: 6 issues
Editorial Board

Current Opinion in Pharmacology

The Current Opinion journals were developed out of the recognition that it is increasingly difficult for specialists to keep up to date with the expanding volume of information published in their subject. In Current Opinion in Pharmacology, we help the reader by providing in a systematic manner:
1. The views of experts on current advances in pharmacology in a clear and readable form.
2. Evaluations of the most interesting papers, annotated by experts, from the great wealth of original publications

Division of the subject into sections
The subject of pharmacology is divided into themed sections, each of which is reviewed once a year. The amount of space devoted to each section is related to its importance.

NeurosciencesCardiovascular and renalRespiratoryMusculoskeletalCancerImmunomodulationAnti-infectives • New technologiesGastrointestinalEndocrine and metabolic diseases

Selection of topics to be reviewed
Section Editors, who are major authorities in the field, are appointed by the Editors of the journal. They divide their section into a number of topics, ensuring that the field is comprehensively covered and that all issues of current importance are emphasised. Section Editors commission reviews from authorities on each topic that they have selected.

Authors write short review articles in which they present recent developments in their subject, emphasising the aspects that, in their opinion, are most important. In addition, they provide short annotations to the papers that they consider to be most interesting from all those published in their topic over the previous year.

Editorial Overview
Section Editors write a short overview at the beginning of the section to introduce the reviews and to draw the reader's attention to any particularly interesting developments.

Ethics in Publishing: General Statement

The Editor(s) and Publisher of this Journal believe that there are fundamental principles underlying scholarly or professional publishing. While this may not amount to a formal 'code of conduct', these fundamental principles with respect to the authors' paper are that the paper should: i) be the authors' own original work, which has not been previously published elsewhere, ii) reflect the authors' own research and analysis and do so in a truthful and complete manner, iii) properly credit the meaningful contributions of co-authors and co-researchers, iv) not be submitted to more than one journal for consideration, and v) be appropriately placed in the context of prior and existing research. Of equal importance are ethical guidelines dealing with research methods and research funding, including issues dealing with informed consent, research subject privacy rights, conflicts of interest, and sources of funding. While it may not be possible to draft a 'code' that applies adequately to all instances and circumstances, we believe it useful to outline our expectations of authors and procedures that the Journal will employ in the event of questions concerning author conduct. With respect to conflicts of interest, the Publisher now requires authors to declare any conflicts of interest that relate to papers accepted for publication in this Journal. A conflict of interest may exist when an author or the author's institution has a financial or other relationship with other people or organizations that may inappropriately influence the author's work. A conflict can be actual or potential and full disclosure to the Journal is the safest course. All submissions to the Journal must include disclosure of all relationships that could be viewed as presenting a potential conflict of interest. The Journal may use such information as a basis for editorial decisions and may publish such disclosures if they are believed to be important to readers in judging the manuscript. A decision may be made by the Journal not to publish on the basis of the declared conflict.

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Best Cited over the last year.

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Vitamin D: Modulator of the immune system

1,25-dihydroxyvitamin D3 (1,25(OH)2D3), the active form of vitamin D, is known to regulate calcium and phosphorus metabolism, thus being a key-player in bone-formation. However 1,25(OH)2D3 also has a physiological role beyond its well-known role in skeletal homeostasis. Here, we describe 1,25(OH)2D3 as an immunomodulator targeting various immune cells, including monocytes, macrophages, dendritic cells (DCs), as well as T-lymphocytes and B-lymphocytes, hence modulating both innate and adaptive…

Volume 10, Issue 4, 01 August 2010, Pp 482-496
Femke Baeke | Tatiana Takiishi | Hannelie Korf | Conny Gysemans | Chantal Mathieu

The role of serotonin receptors in the action of atypical antipsychotic drugs

The main class of atypical antipsychotic drugs (APDs) in current use includes the protypical atypical APD, clozapine, as well as aripiprazole, asenapine, iloperidone, lurasidone, olanzapine, quetiapine, risperidone, and ziprasidone. At clinically effective doses, these agents produce extensive blockade of serotonin (5-HT)2A receptors, direct or indirect stimulation of 5-HT1A receptors, and to a lesser extent, reduction in dopamine (DA) D2 receptor-mediated neurotransmission. This contrasts with…

Volume 11, Issue 1, 01 February 2011, Pp 59-67
H. Y. Meltzer | B. W. Massey

MiRNAs as biomarkers and therapeutic targets in cancer

The knowledge that miRNA expression is frequently dysregulated in cancer has uncovered an entirely new repertoire of molecular factors upstream of gene expression, with exciting potential as novel biomarkers and therapeutic targets in cancer. Exploiting the unique characteristics of these molecules including their stability, tissue specificity, ease of detection and manipulation, will bring clinicians ever closer to achieving the goal of individualized cancer treatment. We present a…

Volume 10, Issue 5, 01 October 2010, Pp 543-550
Helen M. Heneghan | Nicola Miller | Michael J. Kerin

Antiretroviral drugs

In October 2010, it will be exactly 25 years ago that the first antiretroviral drug, AZT (zidovudine, 3'-azido-2',3'-dideoxythymidine), was described. It was the first of 25 antiretroviral drugs that in the past 25 years have been formally licensed for clinical use. These antiretroviral drugs fall into seven categories [nucleoside reverse transcriptase inhibitors (NRTIs), nucleotide reverse transcriptase inhibitors (NtRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs), protease…

Volume 10, Issue 5, 01 October 2010, Pp 507-515
Erik De Clercq

Allostery and population shift in drug discovery

Proteins can exist in a large number of conformations around their native states that can be characterized by an energy landscape. The landscape illustrates individual valleys, which are the conformational substates. From the functional standpoint, there are two key points: first, all functionally relevant substates pre-exist; and second, the landscape is dynamic and the relative populations of the substates will change following allosteric events. Allosteric events perturb the structure, and…

Volume 10, Issue 6, 01 December 2010, Pp 715-722
Gozde Kar | Ozlem Keskin | Attila Gursoy | Ruth Nussinov

Dimerization in GPCR mobility and signaling

Many types of cell surface as well as intracellular DNA-binding receptors exist and function as dimers; formation of homodimers or heterodimers appears to not only provide molecular mechanisms for agonist-induced activation but also increase specificity of ligand recognition and versatility of downstream signaling. G-protein-coupled receptors (GPCRs) were long thought to be an exception, but in recent years a lot of evidence has accumulated that GPCRs also can form dimers, even though it is far…

Volume 10, Issue 1, 01 February 2010, Pp 53-58
Martin J. Lohse

Monoclonal antibody therapeutics: History and future

Over the last three decades, monoclonal antibodies have made a dramatic transformation from scientific tools to powerful human therapeutics. At present, approximately 30 therapeutic monoclonal antibodies are marketed in the United States and Europe in a variety of indications, with sales in the US alone reaching approximately $18.5 billion in 2010. This review describes how antibody engineering has revolutionized drug discovery and what are considered the key areas for future development in the…

Volume 12, Issue 5, 01 October 2012, Pp 615-622
Nicholas A P S Buss | Simon J. Henderson | Mary McFarlane | Jacintha M. Shenton | Lolke De Haan

Role of the adaptive immune system in hypertension

Recent studies have shown that both innate and adaptive immunity contribute to hypertension. Inflammatory cells, including macrophages and T cells accumulate in the vessel wall, particularly in the perivascular fat, and in the kidney of hypertensive animals. Mice lacking lymphocytes are resistant to the development of hypertension, and adoptive transfer of T cells restores hypertensive responses to angiotensin II and DOCA-salt challenge. Immune modulating agents have variable, but…

Volume 10, Issue 2, 01 April 2010, Pp 203-207
David G. Harrison | Antony Vinh | Heinrich Lob | Meena S. Madhur

Intrarenal angiotensin II and its contribution to the genesis of chronic hypertension

The increased activity of intrarenal renin-angiotensin system (RAS) in a setting of elevated arterial pressure elicits renal vasoconstriction, increased sodium reabsorption, proliferation, fibrosis and renal injury. Increases in intrarenal and interstitial angiotensin (Ang) II levels are due to increased AT1 receptor mediated Ang II uptake and stimulation of renal angiotensinogen (AGT) mRNA and protein expression. Augmented proximal tubule AGT production increases tubular AGT secretion and…

Volume 11, Issue 2, 01 April 2011, Pp 180-186
L. Gabriel Navar | Minolfa C. Prieto | Ryousuke Satou | Hiroyuki Kobori

Purinergic signalling and bone remodelling

Accumulating evidence suggests that extracellular nucleotides, signalling through P2 receptors, could play an important role in modulating bone cell function. ATP and other nucleotides can stimulate the formation and resorptive activity of osteoclasts (bone-destroying cells) in addition to inhibiting bone mineralisation by osteoblasts. This review discusses the current understanding of the effects of extracellular nucleotides on skeletal cells. © 2010.

Volume 10, Issue 3, 01 June 2010, Pp 322-330
Isabel R. Orriss | Geoffrey Burnstock | Timothy R. Arnett

Drugs for 'protein clouds': Targeting intrinsically disordered transcription factors

Transcription factors (TFs) are very attractive but difficult drug targets. The difficulties come from several directions including the binding promiscuity of TFs and the intrinsically disordered nature of their binding sites, which often resemble 'protein clouds'. For a long time the targeting of proteins without defined structures was considered infeasible. Data have now emerged showing that selective blocking of specific interactions of intrinsically disordered TFs with their protein binding…

Volume 10, Issue 6, 01 December 2010, Pp 782-788
A. Keith Dunker | Vladimir N. Uversky

Opioid-receptor-heteromer-specific trafficking and pharmacology

Homomerization and heteromerization of 7 transmembrane spanning (7TM)/G-protein-coupled receptors (GPCRs) have been an important field of study. Whereas initial studies were performed in artificial cell systems, recent publications are shifting the focus to the in vivo relevance of heteromerization. This is especially apparent for the field of opioid receptors. Drugs have been identified that selectively target opioid heteromers of the delta-opioid receptor with the kappa and the mu-opioid…

Volume 10, Issue 1, 01 February 2010, Pp 73-79
Richard M. van Rijn | Jennifer L. Whistler | Maria Waldhoer

Pharmacology of TNF blockade in rheumatoid arthritis and other chronic inflammatory diseases

Tumor necrosis factor-alpha (TNF) has been unequivocally validated as a therapeutic target in a number of immune-mediated inflammatory disorders (IMIDs). There is now increasing choice of biologic agents within the class all of which successfully neutralize sTNF. But approaches to TNF inhibition differ and currently include mAbs (infliximab, adalimumab, and golimumab), either chimeric or human in sequence, a PEGylated Fab' fragment (certolizumab), and an IgG1-TNFR2 fusion protein (etanercept).…

Volume 10, Issue 3, 01 June 2010, Pp 308-315
Peter C. Taylor

Selective PDE inhibitors as novel treatments for respiratory diseases

Phosphodiesterases (PDEs) are a family of enzymes which catalyse the metabolism of the intracellular cyclic nucleotides, c-AMP and c-GMP that are expressed in a variety of cell types and in the context of respiratory diseases, It is now recognised that the use of PDE3, PDE4 and mixed PDE3/4 inhibitors can provide clinical benefit to patients with asthma or chronic obstructive pulmonary disease (COPD). The orally active PDE4 inhibitor Roflumilast-n-oxide has been approved for treatment of severe…

Volume 12, Issue 3, 01 June 2012, Pp 275-286
Clive P. Page | Domenico Spina

The role of conformational ensembles of seven transmembrane receptors in functional selectivity

It has been observed that some ligands cause receptors to selectively interact with subsets of signaling proteins to 'bias' their signaling; this is inconsistent with receptors forming a single active state. Here we review the concept of receptor conformation ensembles that can account for a given agonist showing varied efficacies for different signaling pathways. Data show that agonists can stabilize different receptor conformations. We provide a demonstration at the molecular level of how the…

Volume 10, Issue 6, 01 December 2010, Pp 775-781
Nagarajan Vaidehi | Terry Kenakin

Endoplasmic reticulum stress as a progression factor for kidney injury

Dysfunction of endoplasmic reticulum (ER) maintaining protein homeostasis can result from various disturbances, including hypoxia or oxidative stress, which lead to an imbalance between protein-folding capacity and protein-folding load. This in turn leads to ER stress and induction of the unfolded protein response (UPR). The UPR initially serves as an adaptive response, but also induces apoptosis in cells under severe or prolonged ER stress. Accumulating evidence indicates that ER stress…

Volume 10, Issue 2, 01 April 2010, Pp 156-165
Reiko Inagi

Crosstalk between perivascular adipose tissue and blood vessels

Crosstalk between cells in the blood vessel wall is vital to normal vascular function and is perturbed in diseases such as atherosclerosis and hypertension. Perivascular adipocytes reside at the adventitial border of blood vessels but until recently were virtually ignored in studies of vascular function. However, perivascular adipocytes have been demonstrated to be powerful endocrine cells capable of responding to metabolic cues and transducing signals to adjacent blood vessels. Accordingly,…

Volume 10, Issue 2, 01 April 2010, Pp 191-196
Srinivas Rajsheker | David Manka | Andra L. Blomkalns | Tapan K. Chatterjee | Lynn L. Stoll | Neal L. Weintraub

The molecular mechanisms underlying the pharmacological actions of ER modulators: Implications for new drug discovery in breast cancer

Our understanding of the molecular mechanisms underlying the pharmacological actions of estrogen receptor (ER) ligands has evolved considerably in recent years. Much of this knowledge has come from a detailed dissection of the mechanism(s) of action of the Selective Estrogen Receptor Modulators (SERMs) tamoxifen and raloxifene, so called for their ability to function as ER agonists or antagonists depending on the tissue in which they operate. These mechanistic insights have had a significant…

Volume 10, Issue 6, 01 December 2010, Pp 620-628
Donald P. McDonnell | Suzanne E. Wardell

The role of dimerisation in the cellular trafficking of G-protein-coupled receptors

The concept that G-protein-coupled receptors can exist as homomeric and/or heteromeric complexes is now well established. Despite this, how dynamic such interactions are and if this may be modulated during receptor trafficking remain topics of debate. Use of endoplasmic reticulum trapping strategies and the generation of asymmetric homomers have started to provide information on the contribution of protein-protein interactions to receptor maturation, cell surface delivery and ligand-mediated…

Volume 10, Issue 1, 01 February 2010, Pp 23-29
Graeme Milligan

Development of aptamer therapeutics

The field of aptamer research is growing rapidly, with ∼230 papers using the word 'aptamer' published from January to June 2010. These reports cover many different applications ranging from tools to study protein function to potential diagnostic and therapeutic agents. In this review we will focus on the processes involved in isolating and developing aptamers as therapeutic compounds, using specific examples including the first aptamer therapeutic approved for use in humans (Pegaptanib or…

Volume 10, Issue 5, 01 October 2010, Pp 557-562
David H J Bunka | Olga Platonova | Peter G. Stockley

Viral vector-mediated RNA interference

RNA interference (RNAi) is a powerful gene silencing mechanism that if properly harnessed has the potential to revolutionize medical interventions. Delivery of inhibitory RNAs to target tissues needs to be safe, efficient, and for many diseases, long-lasting, in order to exploit this endogenous mechanism for therapeutic purposes. Viral vector systems, based on adeno-associated viruses and lentiviruses, are ideally suited to mediate RNAi because they can safely transduce a wide range of tissues…

Volume 10, Issue 5, 01 October 2010, Pp 534-542
Linda B. Couto | Katherine A. High

Zebrafish as a model for vertebrate hematopoiesis

The zebrafish (Danio rerio) is a model organism making useful contributions in many areas of biological research. Zebrafish have proven particularly suitable for studying early development. The transparency and ex vivo development of zebrafish embryos means that early embryology can be easily visualized, especially using transgenic strains expressing fluorophores marking tissues of interest. High fecundity and tolerance of dense mutagenesis have made it a practical model for forward genetic…

Volume 10, Issue 5, 01 October 2010, Pp 563-570
Felix Ellett | Graham J. Lieschke

Recent advances in bioluminescence resonance energy transfer technologies to study GPCR heteromerization

The field of G protein-coupled receptor (GPCR) research has undergone a transformation in recent years due to the notion of heteromerization. In order to progress our understanding of the functional implications of this phenomenon, as well as its applicability across the diversity of GPCR subtypes, we need to continually look to improve the technologies we use to evaluate protein-protein interactions in as near a physiological setting as possible. The bioluminescence resonance energy transfer…

Volume 10, Issue 1, 01 February 2010, Pp 44-52
Mohammed A. Ayoub | Kevin DG Pfleger

Non-peptide AT2-receptor agonists

The renin-angiotensin-system harbours two main receptor subtypes binding angiotensin II which are the AT1-receptor and the AT2-receptor. While the AT1-receptor has been a drug target in cardiovascular disease for many years, the AT2-receptor was only a subject of academic interest. This has changed with the design and synthesis of a first non-peptide, orally active AT2-receptor agonist, compound 21 (C21). First data using C21 revealed tissue protective effects and functional improvement after…

Volume 11, Issue 2, 01 April 2011, Pp 187-192
U. Muscha Steckelings | Mats Larhed | Anders Hallberg | Robert E. Widdop | Emma S. Jones | Charlotta Wallinder | Pawel Namsolleck | Björn Dahlöf | Thomas Unger

Resolution phase lipid mediators of inflammation: Agonists of resolution

Lipid mediators are appreciated for their roles in leukocyte traffic required in host defense. With identification of novel resolution phase mediators, resolvins, protectins and maresins, these three families and their aspirin-triggered forms, given their potent stereoselective actions with human cells and animal disease models, are coined specialized pro-resolving mediators (SPM). Stereochemistries of key SPM are established and several groups reported organic synthesis. Given increased…

Volume 13, Issue 4, 07 June 2013, Pp 632-640
Charles N. Serhan | Nan Chiang